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dc.contributor.authorNirthanan, S
dc.contributor.authorZiebell, MR
dc.contributor.authorChiara, DC
dc.contributor.authorHong, F
dc.contributor.authorCohen, JB
dc.date.accessioned2017-05-03T15:29:01Z
dc.date.available2017-05-03T15:29:01Z
dc.date.issued2005
dc.date.modified2009-09-28T06:52:27Z
dc.identifier.issn0006-2960
dc.identifier.doi10.1021/bi051209y
dc.identifier.urihttp://hdl.handle.net/10072/25851
dc.description.abstractThe interactions of a photoreactive analogue of benzoylcholine, 4-azido-2,3,5,6-tetrafluorobenzoylcholine (APFBzcholine), with nicotinic acetylcholine receptors (nAChRs) were studied using electrophysiology and photolabeling. APFBzcholine acted as a low-efficacy partial agonist, eliciting maximal responses that were 0.3 and 0.1% of that of acetylcholine for embryonic mouse and Torpedo nAChRs expressed in Xenopus oocytes, respectively. Equilibrium binding studies of [3H]APFBzcholine with nAChR-rich membranes from Torpedo electric organ revealed equal affinities (Keq = 12 卩 for the two agonist binding sites. Upon UV irradiation at 254 nm, [3H]APFBzcholine was photoincorporated into the nAChR a, ?, and d subunits in an agonist-inhibitable manner. Photolabeled amino acids in the agonist binding sites were identified by Edman degradation of isolated, labeled subunit fragments. [3H]APFBzcholine photolabeled ?Leu-109/dLeu-111, ?Tyr-111, and ?Tyr-117 in binding site segment E as well as aTyr-198 in a subunit binding site segment C. The observed pattern of photolabeling is examined in relation to the predicted orientation of the azide when APFBzcholine is docked in the agonist binding site of a homology model of the nAChR extracellular domain based upon the structure of the snail acetylcholine binding protein.
dc.description.peerreviewedYes
dc.description.publicationstatusYes
dc.languageEnglish
dc.language.isoeng
dc.publisherAmerican Chemical Society
dc.publisher.placeWashington, DC
dc.relation.ispartofstudentpublicationN
dc.relation.ispartofpagefrom13447
dc.relation.ispartofpageto13456
dc.relation.ispartofissue41
dc.relation.ispartofjournalBiochemistry
dc.relation.ispartofvolume44
dc.rights.retentionY
dc.subject.fieldofresearchMedicinal and biomolecular chemistry
dc.subject.fieldofresearchBiochemistry and cell biology
dc.subject.fieldofresearchReceptors and membrane biology
dc.subject.fieldofresearchMedical biochemistry and metabolomics
dc.subject.fieldofresearchBasic pharmacology
dc.subject.fieldofresearchcode3404
dc.subject.fieldofresearchcode3101
dc.subject.fieldofresearchcode310110
dc.subject.fieldofresearchcode3205
dc.subject.fieldofresearchcode321401
dc.titlePhotolabeling the Torpedo Nicotinic Acetylcholine Receptor with 4-Azido-2,3,5,6-tetrafluorobenzoylcholine, a Partial Agonist
dc.typeJournal article
dc.type.descriptionC1 - Articles
dc.type.codeC - Journal Articles
gro.date.issued2005
gro.hasfulltextNo Full Text
gro.griffith.authorNirthanan, Niru


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